CN112930180A - 用于跨血脑屏障递送的乙酰化前药 - Google Patents

用于跨血脑屏障递送的乙酰化前药 Download PDF

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CN112930180A
CN112930180A CN201980040860.9A CN201980040860A CN112930180A CN 112930180 A CN112930180 A CN 112930180A CN 201980040860 A CN201980040860 A CN 201980040860A CN 112930180 A CN112930180 A CN 112930180A
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composition
disease
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D·R·埃尔马列
T·M·肖普
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General Hospital Corp
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General Hospital Corp
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0404—Lipids, e.g. triglycerides; Polycationic carriers
    • A61K51/0406—Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
    • A61K51/1279—Plasters, bandages, dressings, patches or adhesives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/56—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
    • C07C217/60—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/26—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C219/28—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton having amino groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dispersion Chemistry (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201980040860.9A 2018-04-20 2019-04-22 用于跨血脑屏障递送的乙酰化前药 Pending CN112930180A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862660365P 2018-04-20 2018-04-20
US62/660,365 2018-04-20
PCT/US2019/028515 WO2019204808A1 (en) 2018-04-20 2019-04-22 Acetylated prodrugs for delivery across the blood-brain barrier

Publications (1)

Publication Number Publication Date
CN112930180A true CN112930180A (zh) 2021-06-08

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CN201980040860.9A Pending CN112930180A (zh) 2018-04-20 2019-04-22 用于跨血脑屏障递送的乙酰化前药

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US (1) US20210238124A1 (de)
EP (1) EP3781149A4 (de)
JP (1) JP2021522196A (de)
KR (1) KR20210005647A (de)
CN (1) CN112930180A (de)
AU (1) AU2019256714A1 (de)
CA (1) CA3097568A1 (de)
WO (1) WO2019204808A1 (de)

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Publication number Priority date Publication date Assignee Title
AU2022428997A1 (en) 2021-12-31 2024-08-15 Imnewrun, Inc. Blood-brain barrier permeable fusion protein and uses thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0333522A2 (de) * 1988-03-18 1989-09-20 MITSUI TOATSU CHEMICALS, Inc. Catechol-Derivate und sie enthaltende pharmazeutische Präparate
WO2006041875A1 (en) * 2004-10-06 2006-04-20 Allergan, Inc. Novel prostamides for the treatment of glaucoma and related diseases
US7186744B2 (en) * 2003-11-13 2007-03-06 Allergan, Inc. Prostamides for the treatment of glaucoma and related diseases
US20120010125A1 (en) * 2010-04-20 2012-01-12 Stone Eric A Methods, compounds and pharmaceutical compositions for treating anxiety and mood disorders
CN103550175A (zh) * 2013-10-15 2014-02-05 海南卫康制药(潜山)有限公司 注射用乙酰谷酰胺组合物冻干粉针
CN104936623A (zh) * 2013-01-24 2015-09-23 泰勒顿国际控股公司 神经元成像与治疗

Family Cites Families (7)

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US4311706A (en) * 1980-01-22 1982-01-19 Interx Research Corporation Novel dopa/dopamine prodrugs
US4506080A (en) * 1983-07-01 1985-03-19 Nestec S. A. Preparation of serotonine and derivatives
US5246949A (en) * 1989-12-06 1993-09-21 Sansho Co., Ltd. Preparation for endermism containing dopamine derivatives
SE0002934D0 (sv) * 2000-08-17 2000-08-17 Axon Biochemicals Bv New aporphine esters and in their use in therapy
EP2289564A3 (de) * 2006-09-08 2012-11-14 Piramal Imaging SA Anilinderivative als Edukte zur F18-Markierung
BR112015022896B1 (pt) * 2013-03-15 2022-08-23 Chongxi Yu Composto de fármacos de alta penetração, composição farmacêutica e seus usos para o tratamento de doenças de parkinson
ES2745529T3 (es) * 2013-10-28 2020-03-02 Bracco Imaging Spa Procedimiento para la preparación de compuestos de carboxilato hiperpolarizado

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0333522A2 (de) * 1988-03-18 1989-09-20 MITSUI TOATSU CHEMICALS, Inc. Catechol-Derivate und sie enthaltende pharmazeutische Präparate
US7186744B2 (en) * 2003-11-13 2007-03-06 Allergan, Inc. Prostamides for the treatment of glaucoma and related diseases
WO2006041875A1 (en) * 2004-10-06 2006-04-20 Allergan, Inc. Novel prostamides for the treatment of glaucoma and related diseases
US20120010125A1 (en) * 2010-04-20 2012-01-12 Stone Eric A Methods, compounds and pharmaceutical compositions for treating anxiety and mood disorders
CN104936623A (zh) * 2013-01-24 2015-09-23 泰勒顿国际控股公司 神经元成像与治疗
CN103550175A (zh) * 2013-10-15 2014-02-05 海南卫康制药(潜山)有限公司 注射用乙酰谷酰胺组合物冻干粉针

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BORIS D.ZLATOPOL SKIY等: "A Practical One-Pot Synthesis of Positron Emission Tomography(PET) Tracers via Nickel-Me diated Radiofluorination" *
CARELLI, VINCENZO等: "New systems for the specific delivery and sustained release of dopamine to the brain" *
MOHAMMAD NAMAVARI等: "Synthesis of 6-[18F]Fluorodopamine,6-[18F]Fluoro-m-Tyramine and 4-[18F]Fluoro-m-Tyramie+" *
QU, MENGKE等: "A brain targeting functionalized liposomes of the dopamine derivative N-3,4-bis(pivaloyloxy)-dopamine for treatment of Parkinson\'s disease" *
REGISTRY: "41265-09-2，48167-07-3，48198-89-6， 67302-27-6" *
庆晓东;唐莉;郑俊青;: "乙酰谷酰胺注射液辅治颅脑损伤昏迷疗效观察" *

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US20210238124A1 (en) 2021-08-05
JP2021522196A (ja) 2021-08-30
EP3781149A4 (de) 2022-03-16
EP3781149A1 (de) 2021-02-24
AU2019256714A1 (en) 2020-11-12
CA3097568A1 (en) 2019-10-24
KR20210005647A (ko) 2021-01-14
WO2019204808A1 (en) 2019-10-24

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